OBJECTIVE To study the pharmacokinetics of picamilon tablet in 12 healthy volunteers. METHODS Picamilon tablets were administrated to healthy volunteers, and plasma concentrations were determined by LC-MS. The pharmacokinetic parameters were calculated. RESULTS The oral dose of 50, 100 and 200 mg were administrated to volunteers. The pharmacokineitc parameters were as follows: tmax (0.73±0.41), (0.67±0.33) and (0.67±0.31)h, t1/2 (0.68±0.22), (0.89±0.41) and (0.91±0.21)h, ρmax (1 328.75±552.33), (2 460.83±571.19) and (4 415.00±1 077.45) μg·L-1, AUC0-tn (1 617.37±575.48), (3 117.08±620.93) and (5 987.01±1 365.57) μg·h·L-1, AUC0-￥ (1 697.45±584.78), (3 227.39±641.54) and (6 192.36±1 388.59) μg·h·L-1, respectively. The plasma concentration-time curves were described by a two compartment open model. CONCLUSION ■AUC and ρmax could be increased with the increased dose. No gender effect on pharmacokinetic parameters was found.